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Research ArticleArticle

Absolute Oral Bioavailability and Metabolic Turnover of β-Sitosterol in Healthy Subjects

Guus Duchateau, Brett Cochrane, Sam Windebank, Justyna Herudzinska, Davindera Sanghera, Angela Burian, Markus Müller, Markus Zeitlinger and Graham Lappin
Drug Metabolism and Disposition October 2012, 40 (10) 2026-2030; DOI: https://doi.org/10.1124/dmd.112.046623
Guus Duchateau
Unilever R&D, Vlaardingen, The Netherlands (G.D.); Unilever Safety & Environmental Assurance Centre, Colworth, United Kingdom (B.C., S.W.); Xceleron Ltd., York, United Kingdom (J.H., D.S., G.L.); and Medical University of Vienna, Vienna, Austria (A.B., M.M., M.Z.)
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Brett Cochrane
Unilever R&D, Vlaardingen, The Netherlands (G.D.); Unilever Safety & Environmental Assurance Centre, Colworth, United Kingdom (B.C., S.W.); Xceleron Ltd., York, United Kingdom (J.H., D.S., G.L.); and Medical University of Vienna, Vienna, Austria (A.B., M.M., M.Z.)
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Sam Windebank
Unilever R&D, Vlaardingen, The Netherlands (G.D.); Unilever Safety & Environmental Assurance Centre, Colworth, United Kingdom (B.C., S.W.); Xceleron Ltd., York, United Kingdom (J.H., D.S., G.L.); and Medical University of Vienna, Vienna, Austria (A.B., M.M., M.Z.)
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Justyna Herudzinska
Unilever R&D, Vlaardingen, The Netherlands (G.D.); Unilever Safety & Environmental Assurance Centre, Colworth, United Kingdom (B.C., S.W.); Xceleron Ltd., York, United Kingdom (J.H., D.S., G.L.); and Medical University of Vienna, Vienna, Austria (A.B., M.M., M.Z.)
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Davindera Sanghera
Unilever R&D, Vlaardingen, The Netherlands (G.D.); Unilever Safety & Environmental Assurance Centre, Colworth, United Kingdom (B.C., S.W.); Xceleron Ltd., York, United Kingdom (J.H., D.S., G.L.); and Medical University of Vienna, Vienna, Austria (A.B., M.M., M.Z.)
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Angela Burian
Unilever R&D, Vlaardingen, The Netherlands (G.D.); Unilever Safety & Environmental Assurance Centre, Colworth, United Kingdom (B.C., S.W.); Xceleron Ltd., York, United Kingdom (J.H., D.S., G.L.); and Medical University of Vienna, Vienna, Austria (A.B., M.M., M.Z.)
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Markus Müller
Unilever R&D, Vlaardingen, The Netherlands (G.D.); Unilever Safety & Environmental Assurance Centre, Colworth, United Kingdom (B.C., S.W.); Xceleron Ltd., York, United Kingdom (J.H., D.S., G.L.); and Medical University of Vienna, Vienna, Austria (A.B., M.M., M.Z.)
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Markus Zeitlinger
Unilever R&D, Vlaardingen, The Netherlands (G.D.); Unilever Safety & Environmental Assurance Centre, Colworth, United Kingdom (B.C., S.W.); Xceleron Ltd., York, United Kingdom (J.H., D.S., G.L.); and Medical University of Vienna, Vienna, Austria (A.B., M.M., M.Z.)
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Graham Lappin
Unilever R&D, Vlaardingen, The Netherlands (G.D.); Unilever Safety & Environmental Assurance Centre, Colworth, United Kingdom (B.C., S.W.); Xceleron Ltd., York, United Kingdom (J.H., D.S., G.L.); and Medical University of Vienna, Vienna, Austria (A.B., M.M., M.Z.)
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Abstract

The metabolic turnover, absolute oral bioavailability, clearance, and volume of distribution for β-sitosterol were measured in healthy subjects. [14C]β-Sitosterol was used as an isotopic tracer to distinguish pulse doses from dietary sources and was administered by both oral and intravenous routes. The administered doses of [14C]β-sitosterol were in the region of 3 to 4 μg, sufficiently low as not to perturb the kinetics of β-sitosterol derived from the diet. Because the plasma concentrations of [14C]β-sitosterol arising from such low doses were anticipated to be very low, the ultrasensitive isotope ratio analytical method of accelerator mass spectrometry was used. The limit of quantification for [14C]β-sitosterol was approximately 0.1 pg/ml, the oral absolute bioavailability was just 0.41%, clearance was 85 ml/h, volume of distribution was 46 L, and the turnover was 5.8 mg/day. Given the steady-state concentrations of β-sitosterol (2.83 μg/ml), then the dietary load was calculated to be approximately 1400 mg/day.

Footnotes

  • Article, publication date, and citation information can be found at http://dmd.aspetjournals.org.

    http://dx.doi.org/10.1124/dmd.112.046623.

  • ABBREVIATIONS:

    AMS
    accelerator mass spectrometry
    ANU
    Australian National University
    AUC
    area under the plasma concentration-time curve
    CL
    clearance
    CV
    coefficient of variation
    GC-MS
    gas chromatography-mass spectrometry
    HPLC
    high-performance liquid chromatography
    LOQ
    limit of quantification
    pMC
    percent modern carbon
    t½
    elimination half-life
    t½α
    t½β, elimination half-lives for the α and β elimination phases, respectively
    V
    volume of distribution
    Vss
    volume of distribution at steady state.

  • Received May 4, 2012.
  • Accepted July 23, 2012.
  • Copyright © 2012 by The American Society for Pharmacology and Experimental Therapeutics
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Drug Metabolism and Disposition: 40 (10)
Drug Metabolism and Disposition
Vol. 40, Issue 10
1 Oct 2012
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Research ArticleArticle

METABOLISM OF SITOSTEROL

Guus Duchateau, Brett Cochrane, Sam Windebank, Justyna Herudzinska, Davindera Sanghera, Angela Burian, Markus Müller, Markus Zeitlinger and Graham Lappin
Drug Metabolism and Disposition October 1, 2012, 40 (10) 2026-2030; DOI: https://doi.org/10.1124/dmd.112.046623

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Research ArticleArticle

METABOLISM OF SITOSTEROL

Guus Duchateau, Brett Cochrane, Sam Windebank, Justyna Herudzinska, Davindera Sanghera, Angela Burian, Markus Müller, Markus Zeitlinger and Graham Lappin
Drug Metabolism and Disposition October 1, 2012, 40 (10) 2026-2030; DOI: https://doi.org/10.1124/dmd.112.046623
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